Abstract: Matrine-family alkaloids as tetracycloquinolizindine analogues from tradition chinese medicine Sophora flavescens Ait, Sophora subprostrata and Sophora alopecuroides L possess various pharmacological activities and have been aroused great interests over the past decades. Especially, plenties of derivatives from matrine-family alkaloids have been synthesized and investigated for their biological activities and encouraging results have continuously acheived in recent several years. These studies are helpful to develop more potent candidates or therapeutic agents and disclose their molecular targets and mechanisms. This review mainly introduces recent advances on the bioactive modifications of matrine-family alkaloids from derivatization at the C-13, C-14 or C-15 position, opening D ring and derivatization, fusing D ring and derivatization and structural simplification based on matrine-family alkaloids
